会员体验
专利管家(专利管理)
工作空间(专利管理)
风险监控(情报监控)
数据分析(专利分析)
侵权分析(诉讼无效)
联系我们
交流群
官方交流:
QQ群: 891211   
微信请扫码    >>>
现在联系顾问~
热词
    • 3. 发明授权
    • Crystalline bortezomib process
    • 结晶硼替佐米方法
    • US09217001B2
    • 2015-12-22
    • US14434105
    • 2013-11-12
    • Vimal Kumar ShrawatRafiuddinVinod Kumar SinghAkshay Kant Chaturvedi
    • Vimal Kumar ShrawatRafiuddinVinod Kumar SinghAkshay Kant Chaturvedi
    • C07D241/12C07F5/02C07F5/04
    • C07F5/025C07B2200/13C07D241/12
    • The present invention provides process for preparation of crystalline Bortezomib (Ia) as its monohydrate which is designated as crystalline Form-SB and characterized by having water content ranging between 3.5-6.0% w/w; X-ray powder diffraction pattern comprising characteristic 2θ° peaks selected from the XRPD peak set of 5.6, 7.5, 9.8, 10.2, 11.3, 15.1, 18.0, 20.5, 21.5 and 23.6±0.20 2θ°, wherein peaks at 9.8 and 11.39±0.20 2θ° are un-split and 100% intensity peak is present at 5.6±0.20 2θ°, DSC isotherm comprising the endothermic peaks ranging between 45 to 60° C. (Peak-1) and 175 to 185° C. (Peak-2) and IR absorption characteristic peaks approximately at 3387 cm−1, 3304 cm−1, 2953 cm−1, 2927 cm−1, 2868 cm−1, 1627 cm−1, 1455 cm−1, 1400 cm−1, 1201 cm−1, 1150 cm−1, 1020 cm−1, 747 cm−1 and 702 cm−1 and Raman absorption spectra having characteristic peaks approximately at 3066 cm−1, 1583 cm−1, 1528 cm−1, 1281 cm−1, 1213 cm−1, 1035 cm−1, 1022 cm−1 and 1004 cm−1. The invention also provides the use of said crystalline Form-SB as active pharmaceutical ingredient in pharmaceutical compositions for the treatment of cancer.
    • 本发明提供制备作为其一水合物的结晶硼替佐米(Ia)的方法,其被称为结晶形式-SB,其特征在于含水量在3.5-6.0%w / w之间; X射线粉末衍射图包含特征2& t s;峰值选自5.6,7.5,9.8,10.2,11.3,15.1,18.0,20.5,21.5和23.6±0.20 2的色度;°,其中9.8和11.39的峰 ±0.20 2& thetas;°是未分裂的,并且在5.6±0.20 2时存在100%强度峰值;°,DSC等温线包含在45至60℃(峰-1)和175至185℃之间的吸热峰。 (峰-2)和IR吸收特征峰值大约在3387cm -1,3304cm -1,2953cm -1,2927cm -1,2868cm -1,1627cm -1,1455cm -1,1400cm -1, 具有大约在3066cm-1,1583cm-1,1528cm -1的特征峰的拉曼吸收光谱的1,1201cm -1,1150cm -1,1020cm -1,747cm -1和702cm -1, 1281cm-1,1213cm-1,1035cm -1,1022cm -1和1004cm -1。 本发明还提供所述结晶形式-SB作为药物组合物中的活性药物成分用于治疗癌症的用途。